G-CSFR Inhibitors
The Granulocyte Colony-Stimulating Factor Receptor (G-CSFR), encoded by the CSF3R gene, is a transmembrane receptor primarily expressed on the surface of hematopoietic stem cells and mature granulocytes. Its primary function is to regulate the production, proliferation, and differentiation of granulocyte lineage cells, including neutrophils, eosinophils, and basophils. Upon binding with its ligand, Granulocyte Colony-Stimulating Factor (G-CSF), G-CSFR activates intracellular signaling cascades, particularly the Janus kinase/signal transducer and activator of transcription (JAK/STAT) pathway, leading to the transcription of genes involved in granulopoiesis and cell survival. G-CSFR signaling also influences other cellular processes such as cell migration, adhesion, and immune response regulation, contributing to the maintenance of innate immunity and host defense against infections.
Inhibiting G-CSFR activity can be achieved through various mechanisms targeting different stages of its signaling pathway. One approach is to block the interaction between G-CSF and its receptor using neutralizing antibodies or small molecule inhibitors, preventing receptor activation and downstream signaling events. Another strategy involves inhibiting the activity of JAK kinases, which are critical mediators of G-CSFR signaling. Small molecule inhibitors targeting JAKs can disrupt the phosphorylation of STAT proteins and subsequent gene transcription, effectively blocking the effects of G-CSF on granulocyte production. Additionally, downstream effectors of G-CSFR signaling, such as transcription factors and survival pathways, can be targeted to inhibit granulocyte differentiation and survival. Overall, inhibition of G-CSFR signaling represents an approach for conditions characterized by excessive granulopoiesis or aberrant immune responses, offering insights into the modulation of hematopoietic processes and immune function.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Eltrombopag | 496775-61-2 | sc-207614 sc-207614A sc-207614B | 5 mg 50 mg 100 mg | $263.00 $381.00 $490.00 | 1 | |
Eltrombopag (SB-497115) is a small-molecule inhibitor targeting the Janus kinase (JAK) pathway. It inhibits JAK2, which is involved in G-CSFR signaling. By blocking JAK2, SB-497115 can disrupt the downstream signaling cascades associated with G-CSFR, leading to its potential inhibition. | ||||||
Cyt387 | 1056634-68-4 | sc-364733 sc-364733A | 10 mg 50 mg | $214.00 $612.00 | 2 | |
CYT387 is a JAK1/JAK2 inhibitor that can interfere with the JAK-STAT signaling pathway. As G-CSFR utilizes the JAK-STAT pathway for signaling, CYT387 may disrupt this pathway, modulating the activation of G-CSFR and potentially acting as an inhibitor. | ||||||
TG101348 | 936091-26-8 | sc-364740 sc-364740A | 5 mg 25 mg | $207.00 $515.00 | 6 | |
TG101348 (Fedratinib) is a JAK2 inhibitor that can potentially interfere with the JAK-STAT signaling pathway used by G-CSFR. Through the inhibition of JAK2, fedratinib may disrupt the downstream signaling cascades associated with G-CSFR, leading to modulation or inhibition of its activity. | ||||||
Ruxolitinib | 941678-49-5 | sc-364729 sc-364729A sc-364729A-CW | 5 mg 25 mg 25 mg | $251.00 $500.00 $547.00 | 16 | |
Ruxolitinib is a JAK1/JAK2 inhibitor that can affect the JAK-STAT pathway. Given the involvement of JAK-STAT signaling in G-CSFR activation, ruxolitinib may interfere with this pathway, potentially inhibiting G-CSFR and disrupting downstream signaling events associated with its activation. | ||||||
AZD1480 | 935666-88-9 | sc-364735 sc-364735A | 5 mg 50 mg | $124.00 $1072.00 | 11 | |
AZD1480 is a JAK1/JAK2 inhibitor with the potential to modulate G-CSFR signaling. By inhibiting JAK2, AZD1480 can interfere with the downstream signaling cascades associated with G-CSFR, potentially acting as an inhibitor and disrupting the intracellular events related to G-CSFR activation. | ||||||
PAC 1 | 315183-21-2 | sc-203174 sc-203174A | 10 mg 50 mg | $132.00 $536.00 | 1 | |
PAC-1 is an activator of procaspase-3, and its action on caspases may impact cellular processes relevant to G-CSFR signaling. By influencing caspase activity, PAC-1 can potentially modulate pathways associated with G-CSFR, leading to the inhibition or modulation of G-CSFR activity. | ||||||
BX 795 | 702675-74-9 | sc-281689 sc-281689A sc-281689C sc-281689B sc-281689D sc-281689E | 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg | $219.00 $273.00 $331.00 $495.00 $882.00 $1489.00 | 5 | |
BX-795 is an inhibitor of PDK1 (3-phosphoinositide-dependent protein kinase 1), a kinase involved in multiple signaling pathways. By inhibiting PDK1, BX-795 can potentially impact G-CSFR-related signaling pathways, leading to the modulation or inhibition of G-CSFR activity. | ||||||
TGF-β RI Kinase Inhibitor V | 627536-09-8 | sc-203294 | 2 mg | $88.00 | 3 | |
TGF-β RI Kinase Inhibitor V (SD-208) is a potent inhibitor of TGF-β receptor I (ALK5). TGF-β signaling can crosstalk with pathways involved in G-CSFR activation. By inhibiting ALK5, SD-208 may interfere with this crosstalk, potentially modulating G-CSFR-related signaling pathways and acting as an inhibitor of G-CSFR. | ||||||
PI 3-Kβ Inhibitor VI, TGX-221 | 663619-89-4 | sc-203190 | 1 mg | $437.00 | ||
TGX-221 is a selective PI3K inhibitor, and its action on the PI3K pathway may impact cellular processes relevant to G-CSFR signaling. By inhibiting PI3K, TGX-221 can potentially modulate pathways associated with G-CSFR, leading to the inhibition or modulation of G-CSFR activity. | ||||||
PD 0332991 Isethionate | 827022-33-3 | sc-478943 | 1 mg | $300.00 | ||
PD 0332991 is a cyclin-dependent kinase (CDK) inhibitor. Its action on CDKs can impact the cell cycle and cellular processes associated with G-CSFR signaling. By influencing the cell cycle, PD 0332991 may modulate pathways relevant to G-CSFR, potentially acting as an inhibitor of G-CSFR. | ||||||